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Pharmaceutical Combination

a technology of combination and medicine, applied in the field of pharmaceutical combination, can solve the problems of unacceptably high incidence of side effects, significant burden on the quality of life of patients, and complex symptoms, and achieve the effect of increasing potency and efficacy

Active Publication Date: 2016-12-20
B3AR THERAPEUTICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes a new treatment for overactive bladder that combines a beta-3 adrenergic receptor agonist and a muscarinic receptor antagonist. This combination has been found to have increased potency and efficacy compared to either component alone. The treatment can be used in a single dosage form or separately, and can be administered to mammals to relieve symptoms associated with overactive bladder. The technical effect of this combination is to provide a more effective treatment for overactive bladder with a synergistic effect that can provide better results for patients.

Problems solved by technology

The underlying pathophysiology is the interruption of the otherwise orderly control of micturition, resulting in the symptom complex described above.
OAB represents a significant quality of life burden to patients.
In particular there is an unacceptably high incidence of side effects, including dry mouth and constipation associated with these medications.
Also, current medications do not adequately treat urgency, one of the most bothersome symptoms of OAB.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

Drug Interaction Study with Healthy Human Subjects

[0143]A drug interaction study was conducted in healthy human volunteers, using repeat oral doses of solabegron and oxybutynin administered singly as well as in combination with each other, in order to assess the effects on pharmacokinetic and pharmacodynamic parameters, as measured by post void residual (PVR) volumes. PVR was measured in subjects treated with each agent alone as well as in combination at steady-state.

[0144]The study was a two-cohort randomized, open label, repeat dose, 3-way crossover study in healthy adult subjects. Two marketed formulations of oxybutynin were used in the study: i) Ditropan IR®, which is immediate release (IR) oxybutynin; and ii) Ditropan XL® which is extended release (XL) oxybutynin. The total daily dose given was 20 mg. Solabegron was administered as tablets. Details of the solabegron tablet composition used are provided in Table 1 (composition A).

[0145]The first cohort (n=14 subjects) was given ...

example 2

Effects of the Combination of Beta-Adrenoceptor Agonists and Antimuscarinics on Bladder Contractility in Rats

[0164]Stimulation of efferent nerves to the urinary bladder results in the release of acetylcholine (ACh) that stimulates post-junctional muscarinic (M3) receptors on urinary bladder smooth muscle, resulting in contraction and subsequent urination. M2 receptors are functionally expressed in human bladder smooth muscle and may also play a role in bladder contractility, however most likely indirectly by enhancing M3 mediated contractions and inhibiting β-adrenoceptor mediated relaxation. Antimuscarinic drugs are believed to work primarily by blocking M3 receptors, thus inhibiting the contractions associated with overactive bladder.

[0165]Another approach to treating overactive bladder involves targeting β3-adrenoceptors, which are also located on urinary bladder smooth muscle. The stimulation of post-junctional β3-adrenoceptors results in the generation of cAMP and production of...

example 3

Effects of the Combinations of Various Beta-Adrenoceptor Agonists and Antimuscarinics on Rat Bladder Contractions Induced by EFS (Electrical Field Stimulation)

[0174]In this study various combinations of β3-adrenoceptor agonists and antimuscarinics were tested in isolated rat urinary bladder strips.

[0175]Urinary bladder smooth muscle strips were obtained from female rats (Sprague-Dawley strain, body weight 240-360 g). Two strips per bladder were prepared and connected to tension transducers in 5 ml organ baths containing Krebs-Henseleit solution (kept at 37° C., pH 7.4, gassed with 95% O2 / 5% CO2). Prazosin (1 μM) was added to the Krebs solution in order to block α1-adrenoceptors. Strips were equilibrated for at least 60 min at 1.0 g resting tension, during which tissues were washed every 15 min. Then, each strip was exposed to 80 mM KCl to verify its viability. After another 45 min wash-out period, strips were subjected to EFS (electrical field stimulation parameters: constant curren...

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Abstract

Pharmaceutical combinations comprising a beta-3 adrenergic receptor agonist and a muscarinic receptor antagonist, and methods for their use are disclosed. Methods of using the pharmaceutical combinations for the treatment of one or more symptoms associated with overactive bladder, for example, frequency of urgency, nocturia, and urinary incontinence, are also disclosed.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]The present application is a Continuation-in-Part under 35 U.S.C. 120 of U.S. patent application Ser. No. 13 / 196,068, filed on Aug. 2, 2011, which claims the benefit of priority under 35 U.S.C. 119(e) of U.S. Provisional Application 61 / 370,171 filed on Aug. 3, 2010. The present application also claims the benefit of priority under 35 U.S.C. 119(e) of U.S. Provisional Application No. 61 / 596,893, filed on Feb. 9, 2012. The entire disclosures of all of the above applications are incorporated herein by reference.FIELD OF THE INVENTION[0002]The present invention relates to pharmaceutical combinations and methods for their use. In particular, the invention relates to pharmaceutical combinations comprising a beta-3 adrenergic receptor agonist and a muscarinic acetylcholine receptor antagonist (hereinafter referred to as “muscarinic receptor antagonist” or “antimuscarinic”), and to methods of using such combinations in the treatment of one or mor...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): A61K31/135A61K31/16A01N43/04A61K31/70A61K31/216A61K31/7024A61K31/13A01N33/00A01N33/02A61K31/426A61K31/196A61K45/06A61K31/137A61K31/357A61K31/4725A61K31/351
CPCA61K31/216A61K31/137A61K31/196A61K31/351A61K31/357A61K31/426A61K31/4725A61K31/7024A61K45/06A61K2300/00A61K9/0053
Inventor CALTABIANO, STEPHENOHLSTEIN, ELIOTMCCALLUM, STEWART
Owner B3AR THERAPEUTICS INC
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